MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

CP671305

CAS No. : 445295-04-5

MCE 站：CP671305

产品活性：CP671305 是一种有效的，可口服的，选择性的 phosphodiesterase-4-D 抑制剂，具有很高的活性。

研究领域：Metabolic Enzyme/Protease

作用靶点：Phosphodiesterase (PDE)

In Vitro: CP-671,305 is identified as a substrate of MRP2 and BCRP, but not MDR1. CP-671,305 is a substrate of human OATP2B1 with a high affinity (K_m=4 μM) but not a substrate for human OATP1B1 or OATP1B3. CP-671,305 displays high affinity (K_m=12 μM) for rat hepatic Oatp1a4. CP-671,305 does not exhibit competitive inhibition of the five major cytochrome P450 enzymes, namely CYP1A2, 2C9, 2C19, 2D6 and 3A4 (IC₅₀s >?50 μM). Likewise, no time-dependent inactivation of the five major cytochrome P450 enzymes is discernible with CP-671,305.

In Vivo: CP-671,305 pharmacokinetics are largely unaltered, and compromised biliary clearance of CP-671,305 is compensated by increased urinary clearance. CP-671,305 demonstrates generally favourable pharmacokinetic properties, systemic plasma clearance after intravenous administration is low in Sprague-Dawley rats (9.60?±?1.16?mL/min/kg), beagle dogs (2.90?±?0.81?mL/min/kg) and cynomolgus monkeys (2.94?±?0.87?mL/min/kg) resulting in plasma half-lives >?5?h. Moderate to high bioavailability in rats (43-80%), dogs (45%) and monkeys (26%) is observed after oral dosing. In rats, oral pharmacokinetics are dose dependent over the dose range studied (10 and 25?mg/kg).

相关产品：Bioactive Compound Library Plus  |  Metabolism/Protease Compound Library  |  Orally Active Compound Library  |  Anti-Alzheimer’s Disease Compound Library  |  IBMX  |  Bucladesine sodium  |  Rolipram  |  Sildenafil  |  Theophylline  |  Icariin  |  Roflumilast  |  Tadalafil  |  PF-04957325  |  Milrinone  |  Dipyridamole  |  Pentoxifylline  |  Cilostazol  |  Ibudilast  |  Butein  |  Cilomilast  |  Cilostamide  |  EHNA hydrochloride  |  Zardaverine  |  Vardenafil hydrochloride  |  Vinpocetine  |  W-7 hydrochloride  |  BRL-50481  |  HA130  |  Aminophylline  |  Pimobendan  |  Anagrelide hydrochloride  |  Bay 60-7550

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。